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Obeticholic Acid

(CAS No:459789-99-2)

Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Phase 3.

CAS No:459789-99-2

Molecular Weight(MW):420.63

Purity:98%+

Specification:500mg;1g;5g;10g;50g;100g

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COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	459789-99-2
Molecular formula(MF)	C₂₆H₄₄O₄
Molecular Weight(MW):	420.63
Alias

Solubility

In vitro	DMSO	84 mg/mL (199.7 mM)
	Ethanol	84 mg/mL warmed (199.7 mM)
	Water	<1 mg/mL
In vivo

Biological Activity

Description

Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Phase 3.

Targets

FXR ^[1]

99 nM(EC50)

In vitro

In HuH7 cells, Obeticholic Acid acts as a potent FXR agonist with EC50 of 85 nM. ^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
COS1 cells	Function assay			Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay, EC50=99 nM	20014870
HeLa cells	Function assay		24 h	Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay, EC50=0.16 Î¼M	25934227
CHO cells	Function assay		5 h	Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay, EC50=0.755 Î¼M	17685603
NCI-H716 cells	Function assay			Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay, EC50=20 Î¼M	21459580
mouse GLUTag cells	Function assay			Agonist activity at GP-BAR1 in mouse GLUTag cells assessed as increase in intracellular cAMP level	24387325
human HepG2 cells	Function assay	10 Î¼M	18 h	Agonist activity at FXR in human HepG2 cells assessed as upregulation of SHP mRNA expression at 10 uM after 18 hrs by RT-PCR analysis	24387325
mouse primary hepatocytes	Function assay			Agonist activity at FXR in mouse primary hepatocytes assessed as upregulation of BESP mRNA expression	24387325

... Click to View More Cell Line Experimental Data

In vivo

In rat cholestasis model, Obeticholic Acid promotes bile flow, and protects hepatocytes against acute necrosis caused by LCA. ^[1] Obeticholic Acid (p.o.) improves proteinuria, ameliorates renal structural changes, and modulates renal inflammation and oxidative stress in WD-fed DBA mice. ^[2] In thioacetamide (TAA)-intoxicated and bile-duct-ligated (BDL) rats, Obeticholic Acid (30 mg/kg p.o.) reactivates the FXR downstream signaling pathway and decreases portal pressure by lowering total IHVR without deleterious systemic hypotension. ^[3]